Abstract: This invention provides compounds of formula 1, having the structure wherein R1, R2, R3, R4, and R5 are described within the specification.

Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.

Abstract: This invention provides compounds of formula 1, having the structure wherein R1, R2, R3, R4, and R5 are described within the specification.

Abstract: The present invention relates to Benzo[c][2,7]naphthyridine Derivatives, compositions comprising an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for modulating PDK-1 activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c][2,7]naphthyridine Derivative.

Abstract: The present invention relates to a method of identifying an inhibitor of a receptor tyrosine kinase that irreversibly binds to the kinase. Specifically, the method comprises using a variety of assays, either alone or in combination, to identify compounds that irreversibly bind to tyrosine kinases. More specifically, there are four assays, which are novel variations of a basic enzyme assay and identify irreversible binding inhibitors.

Abstract: The present invention relates to pyrimido[5,4-c]quinoline-2,4-diamine derivatives, compositions comprising an effective amount of a Pyrimido[5,4-c]quinoline-2,4-diamine Derivative, methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of an Pyrimido[5,4-c]quinoline-2,4-diamine Derivative, methods for modulating PDK-1 activity, comprising administering to a subject in need thereof an effective amount of a Pyrimido[5,4-c]quinoline-2,4-diamine Derivative. The invention also relates to a process for preparing a Pyrimido[5,4-c]quinoline-2,4-diamine Derivative.

Abstract: This invention provides compounds of formula 1, having the structure wherein R1, R2, R3, R4, and R5 are described within the specification.

Abstract: The present invention provides for compounds with the general formula: A compound of formula (1) having the structure (1) wherein Z is a radical selected from the group (a), (b), or (c) as well as methods and compositions containing these compounds useful for treatment of diseases that are characterized, at least in part, by excessive, abnormal, or inappropriate angiogenesis. These disease states, include but are not limited to, cancer, diabetic retinopathy, macular degeneration and rheumatoid arthritis. These compounds inhibit angiogenesis by inhibiting a tyrosine kinase receptor enzyme, specifically KDR, and binding to the KDR in an irreversible manner.

Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.

Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.

Abstract: The present invention is directed to a method of synthizing compounds of formula (I): wherein X, Z, V, R1, R3, R4, G2, n, x, y, and z are defined herein. This invention also includes a method of preparing acid compounds of formula (VII): wherein R is H, and R4, x, y, and z are as defined herein and PG is a protecting group. This invention is also directed to (E)N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(methylamino)-2-butenamide, compositions containing it and methods of using the to treat cancer.

Abstract: This invention provides compounds of formula 1, having the structure which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.

Abstract: This invention provides compounds of formula 1, having the structure which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.

Abstract: This invention provides compounds of formula 1, having the structure wherein R1, R2, R3, R4, and R5 are described within the specification.

Abstract: This invention provides compounds of Formula (I), represented by the structure wherein G1, G2, G3, G4, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.

Abstract: This invention provides compounds of Formula (I), having the structure 1

Abstract: This invention provides compounds of formula 1, having the structure 1

Abstract: This invention provides compounds of Formula (I), having the structure where T, Z, X, A, R1, R2a, R2b, R2c, R3, R4, and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.

Abstract: This invention provides compounds of formula 1, having the structure which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.

Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.